BCX 1470
(Synonyms: 2-(氨基亚氨基甲基)苯并[B]噻吩-6-基-2-噻吩羧酸酯) 目录号 : GC35481BCX 1470能抑制factor D和C1s的酯水解活性,IC50分别为96 nM和1.6 nM。
Cas No.:217099-43-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat.
[1]. Szalai, Alexander J.; Digerness, Stanley B.; et al.; The Arthus Reaction in Rodents: Species-Specific Requirement of ComplementJournal of Immunology, 2000, 164, 463-468
Cas No. | 217099-43-9 | SDF | |
别名 | 2-(氨基亚氨基甲基)苯并[B]噻吩-6-基-2-噻吩羧酸酯 | ||
Canonical SMILES | N=C(C1=CC2=CC=C(OC(C3=CC=CS3)=O)C=C2S1)N | ||
分子式 | C14H10N2O2S2 | 分子量 | 302.37 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.3072 mL | 16.536 mL | 33.0721 mL |
5 mM | 0.6614 mL | 3.3072 mL | 6.6144 mL |
10 mM | 0.3307 mL | 1.6536 mL | 3.3072 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The Arthus reaction in rodents: species-specific requirement of complement
J Immunol 2000 Jan 1;164(1):463-8.PMID:10605043DOI:10.4049/jimmunol.164.1.463
We induced reverse passive Arthus (RPA) reactions in the skin of rodents and found that the contribution of complement to immune complex-mediated inflammation is species specific. Complement was found to be necessary in rats and guinea pigs but not in C57BL/6J mice. In rats, within 4 h after initiation of an RPA reaction, serum alternative pathway hemolytic titers decreased significantly below basal levels, whereas classical pathway titers were unchanged. Thus the dermal reaction proceeds coincident with systemic activation of complement. The serine protease inhibitor BCX 1470, which blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat. These data support the proposal that complement-mediated processes are of major importance in the Arthus reaction in rats and guinea pigs, and suggest that BCX 1470 will be useful as an anti-inflammatory agent in diseases where complement activation is known to be detrimental.